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Submit ReviewAS 1842856 is a potent and selective Foxo1 inhibitor (IC50 values are 33 nM at Foxo1 and >1 μM at Foxo3a and Foxo4); decreases Foxo-mediated promoter activity by 70%, 20% and 3% at Foxo1, Foxo4 and Foxo3, respectively. Regulates gluconeogenesis both in vitro and in vivo. Attenuates fasting plasma glucose level in diabetic db/db mice. Also suppresses autophagy, adipocyte differentiation and soluble guanylyl cyclase expression. Also inhibits STAT3 signaling in NSCLC. Orally bioavailable.
分子量 | 347.39 |
公式 | C18H22FN3O3 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 836620-48-5 |
PubChem ID | 72193864 |
InChI Key | MOMCHYGXXYBDCD-UHFFFAOYSA-N |
Smiles | CCN1C=C(C(C2=C(C(F)=C(C=C12)NC3CCCCC3)N)=O)C(O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 1.74 | 5 温和加热 |
以下数据基于产品分子量 347.39。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.05 mM | 57.57 mL | 287.86 mL | 575.72 mL |
0.25 mM | 11.51 mL | 57.57 mL | 115.14 mL |
0.5 mM | 5.76 mL | 28.79 mL | 57.57 mL |
2.5 mM | 1.15 mL | 5.76 mL | 11.51 mL |
参考文献是支持产品生物活性的出版物。
Nagashima et al (2010) Discovery of novel forkhead box O1 inhibitors for treating type 2 diabetes: improvement of fasting glycemia in diabetic db/db mice. Mol.Pharmacol. 78 961 PMID: 20736318
Liu et al (2016) FoxO1 antagonist suppresses autophagy and lipid droplet growth in adipocytes. Cell Cycle 15 2033 PMID: 27260854
Galley et al (2019) Antagonism of forkhead box subclass O transcription factors elicits loss of soluble guanylyl cyclase expression. Mol.Pharmacol. 95 629 PMID: 30988014
If you know of a relevant reference for AS 1842856, please let us know.
关键词: AS 1842856, AS 1842856 supplier, AS1842856, Potent, selective, FOXO1, inhibitors, inhibits, gluconeogenesis, diabetic, diabetes, orally, bioavailable, forkhead, box, O, family, soluble, guanylyl, cyclase, autophagy, differentiation, adipocytes, Other, Transcription, Factors, Guanylyl, Cyclase, Differentiation, Products, Autophagy, 4265, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AS 1842856 的部分引用包括:
Hye Jung et al (2022) P2Y2R-Mediated PAK1 Activation Is Involved in ESM-1 Overexpression in RT-R-MDA-MB-231 through FoxO1 Regulation. Cancers (Basel) 14 PMID: 36077661
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